The optimized molecular structure, vibrational frequencies, corresponding vibrational assignments of Methyl N-({[2-(2-methoxyacetamido)-4-(phenylsulfanyl) phenyl]amino} [(methoxycarbonyl)imino]methyl)carbamate have been investigated using HF and DFT levels of calculations. The geometrical parame...
Guanosine-5′-triphosphate (GTP) binds specifically to syncytiotrophoblast plasma membranes and increases the production of cyclic AMP in these membranes. 1.1. In syncytiotrophoblast membranes, GTP alone caused a significant increase in the basal levels of cyclic AMP in dose dependent manner.2.2...
A series of new benzazepines with modification on the catecholic fragment were designed. The 8-hydroxyl group, other than the 7-hydroxyl was confirmed crucial to the interaction with the dopamine D1 receptor. Subsequent replacement of the 7-hydroxyl with benzylamino groups was found tolerable. 7...
Two new coumarin derivatives, 7-(N,N′-diethylamino)-3-(4-hydroxyphenyl)-coumarin and 7-(N,N′-diethylamino)-3-(4-bromophenyl)-coumarin, were synthesized successfully. Their structures were verified by single crystal X-ray crystallography. The UV–vis absorption and fluorescence of the compounds...
2-(2′-hydroxyphenyl)iminomethylbenzimidazole(1) and its derivative 2-(2′-hydroxy-4-bromo-phenyl)iminomethylbenzimidazole (2), have been sythesised and their ground and excited-state properties were studied. These compounds show ground-state keto-enol tautomerism. The bromo-substituent in compo...
A series of N-(tert-butoxycarbonyl)-3-[2-(phenyl)benzoxazol-5-yl]alanine methyl ester derivatives possessing electron-donor and electron-acceptor substitutents in the phenyl ring were synthesized and their photophysical properties in methanol, acetonitrile and methylcyclohexane were studied by m...
Allyl 4,6-O-ethylidene-β-d-glucopyranoside is an intermediate used in the synthesis of etoposide phosphate, a water-soluble derivative of the antineoplastic drug etoposide. In this paper, a method for the determination of allyl 4,6-O-ethylidene-β-d-glucopyranoside and related glucopyranosides ...
To improve the solubility and dissolution rate of etoposide, micro-particles were prepared using solution-enhanced dispersion by supercritical CO2, and the transition of crystal form was investigated using scanning electron microscopy, X-ray diffraction, thermogravimetric analysis, and different...
ObjectiveTo evaluate the physical and chemical stability of etoposide phosphate solutions over 7 days at 32°C and 31 days at 4°C and 23°C: (1) at etoposide concentrations of 0.1 and 10 mg/mL as phosphate in 0.9% sodium chloride injection and 5% dextrose injection and (2) at etoposide concentr...
Etoposide phosphate is a water-soluble prodrug of etoposide. A phase I and pharmacokinetic study has been performed over the dose range 25–110 mg/m2/day for 5 days (etoposide equivalent doses). The maximum tolerated dose (MTD) was 110 mg/m2/day for 5 days every 3 weeks and the dose-limiting tox...
High-risk neuroblastoma requires surgical resection and multi-drug chemotherapy. This study aimed to develop an extended release, implantable and degradable delivery system for etoposide, commonly used for neuroblastoma treatment. Different concentrations of silk, a biodegradable, non-toxic, non...
Etoposide phosphate, a water soluble prodrug of etoposide, has several potential advantages including easier and more rapid administration, avoidance of large fluid loads, and elimination of hypersensitivity reactions and other problems related to the solubilizer. This randomized Phase II study ...
The present study was to develop etoposide loaded solid lipid nanoparticles (SLN) and optimize it for effective ocular delivery to the posterior eye. SLN were prepared by melt-emulsification and ultrasonication technique. Etoposide loaded SLN were optimized by using three-factor three levels Box...
In this article, we have reported the inclusion complex behaviors and their pharmaceutical application of anticancer drug property of Etoposide with β-cyclodextrin. The inclusion complex is used to improve the poor aqueous solubility of the anticancer drug Etoposide. The aqueous solubility and ...
A dependable in vitro in vivo correlation (IVIVC) is a vital tool to optimize drug formulation and expedite product development time. Although many IVIVC examples are available for oral delivery systems, IVIVC for transdermal delivery is far less common, especially for electrical-assisted delive...
Cancer chemotherapy frequently requires long periods of multiple intravenous infusions that often results in patients opting out of treatment. The main purpose of this study was to investigate the feasibility of delivering one of these anticancer agents: etoposide phosphate (ETP) transdermally u...
Langmuir-Blodgett films of 2-docosylamino-5-nitropyridine (DCANP) have been introduced as non-centrosymmetric multilayers which exhibit strong second harmonic generation (SHG). Both polarized UV-visible spectroscopy and SHG show preferential orientation with respect to the dipping direction. Fro...
We demonstrate that a significant in-plane anisotropy is present in monolayers of 2-docosylamino-5-nitropyridine at an air-water interface. The floating monolayers were studied by in situ transmission second-harmonic generation under normal incidence and shown to have C1h symmetry. The formation...
2-Docosylamino-5-nitropyridine (DCANP) is a strongly nonlinear optical molecule which forms high optical quality Langmuir-Blodgett (LB) films. DCANP shows higher nonlinearities as compared to its aliphatic chain derivatives (C18H37 to C26H53). To explain this we determined the orientation of the...
Molecules of 2-docosylamino-5-nitropyridine, NO2-C5H3N-NH-C22H45 in a multilayer Langmuir-Blodgett film are ordered in the same direction with the same directional sense. All over the film the -NO2 group is pointing opposite to the dipping direction. This ordering is solely determined by the dip...
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